Cefdinir colon-positioning enteric tablet

A technology of cefdinir and nicolon, applied in the new field of medicine, to achieve the effect of improving therapeutic effect, reducing side effects and improving compliance

Inactive Publication Date: 2009-07-01
BEIJING HOPE HUGE PHARM SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] According to reports by Watanabe et al., in vitro antibacterial experiments have proved that after years of clinical use of cefdinir, its antibacterial activity against major clinical pathogens has not decreased.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1 pH-controlled cefdinir colon-localized preparation,

[0027] Tablet core formula 1

[0028] Cefdinir 100g

[0029] Sodium carboxymethyl starch 6g

[0030] Lactose 30g

[0031] Povidone 2.5g

[0032] Talc powder 4.5g

[0033] 75% ethanol solution 50ml

[0034] Tablet core formula 2

[0035] Cefdinir 100g

[0036] Sodium carboxymethyl starch 6g

[0037] Starch 30g

[0038] Povidone 3.5g

[0039]Magnesium Stearate 4.5g

[0040] 75% ethanol solution 50ml

[0041] Tablet core formulation 3

[0042] Cefdinir 100g

[0043] Low-substituted hydroxypropyl methylcellulose 15g

[0044] Starch 20g

[0045] Methylcellulose 3g

[0046] Talc powder 7.5g

[0047] 75% ethanol solution 50ml

[0048] Tablet core formulation 4

[0049] Cefdinir 200g

[0050] Low-substituted hypromellose 15g

[0051] Lactose 20g

[0052] Povidone 3g

[0053] Micronized silica gel 7.5g

[0054] Acetone 50ml

[0055] Coating Solution Formula 1

[0056] Acrylic resin S100 10g...

Embodiment 2

[0075] Example 2 Time-controlled cefdinir colon-localized drug release preparation

[0076] Tablet core formula is with embodiment 1.

[0077] Preparation of time-controlled coating solution: dissolve the acrylic resin in a solvent and add other components and stir evenly.

[0078] Tablet cores are coated in multiple layers. The composition of the inner coating liquid is 8 g of hypromellose, and the solvent is 200 ml of 70%-90% ethanol. The sub-outer coating solution is composed of 3 g of ethyl cellulose, 0.3 g of hypromellose, and 100 ml of ethanol with a solvent content of 70%-90%. By controlling the thickness of the film, the time lag is adjusted. The release time lag is 3-4 hours. The outermost layer is coated with ethanol solution of acrylic resin L100. Through the dissolution test, the results showed that the coated tablet began to dissolve in the small intestine, and the release time lag was 3.5 hours.

Embodiment 3

[0079] Example 3 Time-controlled and pH-dependent colon-localized formulations

[0080] Tablet core formula is with embodiment 1.

[0081] Time control layer coating solution formula 1:

[0082] Acrylic resin E100 50g

[0083] Povidone 15g

[0084] Macrogol 6000 5g

[0085] Ethanol 500ml

[0086] pH control layer coating solution formula 1:

[0087] Acrylic L100 8g

[0088] Acrylic resin S100 2g

[0089] Diethyl phthalate 4ml

[0090] Castor oil 6ml

[0091] Tween-80 2ml

[0092] Talc powder 6g

[0093] Ethanol 200ml

[0094] Time control layer coating liquid formula 2

[0095] Ethylcellulose 25g

[0096] Hypromellose 5g

[0097] Macrogol 6000 5g

[0098] Ethanol 500ml

[0099] pH control layer coating liquid formula 2

[0100] Acrylic S100 30g

[0101] Triethyl citrate 5g

[0102] Talc powder 7.5g

[0103] Ethanol 500ml

[0104] The preparation method of the pH-controlled coating liquid formulation is the same as in Example 1, and the preparation method o...

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PUM

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Abstract

The invention discloses cefdinir colon-specific enteric-coated tablets, comprising tablet cores and coating layers. The tablet cores are composed of 10-90 wt.% of cefdinir, 2-70 wt.% of diluting auxiliary materials, 1-20 wt.% of disintegrating auxiliary materials, 1-20 wt.% of adhering auxiliary materials and 0.1-5 wt.% of lubricant auxiliary materials. The cefdinir colon-specific enteric-coated tablets can transmit medicament to colons, improve curative effect of colonitis, have low side effect and improve compliance of patients.

Description

technical field [0001] The invention belongs to the field of new medicine technology, and in particular relates to cefdinir colon-localized enteric-coated tablets. For the treatment of colitis. Background technique [0002] Cefdinir (cefdinir) is the third-generation oral cephalosporin developed by Fujisawa Company in Japan. It not only maintains high stability to β-lactamase, but also improves the performance of third-generation cephalosporins such as cefixime. only for G - Bacterial effect is strong, but for G + It has the characteristics of broad antibacterial spectrum, high curative effect and low toxicity. It was first launched in Japan in December 1991 under the product name . In December 1997, it was approved by the FDA to go on the market in the United States under the trade name . It was launched in South Korea in 1999. In 2001, Cefdinir Capsules produced by Tianjin Central Pharmaceutical Co., Ltd. was launched in China. The trade name is Shifu . [0003...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/546A61K9/32A61K47/36A61K47/38A61P31/04
Inventor 王翰斌
Owner BEIJING HOPE HUGE PHARM SCI
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